Agent for the treatment of mucous surfaces



Patented Apr. 19, 1938 UNITED STATES PATENT OFFICE .AGENT FOR. THETREATMENT OF MUCOUS SURFACES Frank J. Bickenheuser,

Tulsa, Okla", assignor, by

,No Drawing.

Application May 26, 1937,

serial No. 144,961

- Claims.

The present invention relates to topical medicines containing, as avehicle, a liquid oily material which has the property of mixing withwater or with moist secretions of the mucous surfaces 5 of the humanbody, to produce a jelly-like mass,

which will be capable of readily adhering to wet mucous surfaces, forany desired period of time.

vehicle, a suitable antiseptic material, and a widevariety of antisepticmaterials can be used, and

in widely varying amounts, so long as the said antiseptic can be gotteninto solution in the said vehicle.

The following is given as the for use in the present case- 2 preferredvehicle Volume Triethanolamine 1 26 Oleic arid 3 Purified mineral oil3.5

,The amount of the oleic acid can be varied, usually between 2.5. and3.5 volumes, and the amount of the mineral oil can be varied, usuallybetween 3 and 4 volumes. But even somewhat wider variation in theproportions may be advantageous in some instances. In place of the abovemineral oil, it is often advisable to employ 35 a mixture of mineral oiland a fatty oil, to thereby iorm jellies of different consistencies,suitable for some specific purpose. substitution. one part of mineraloil can readily be replaced by about 1.2 to 1.4 parts of fatty oil.

In general the ratio of the total amount of the oil used (petroleum oilwith or without fatty oil) to the combined amount of triethanolamine andfree oleic acid (or triethanolamine oleate) is between 0.75:l and 1.2:1.Variation in these ratios 45 modifies the properties of the Jelly, i. e.softness,

toughness, adherence to mucous surfaces, elasticity. The petroleum oilis in excess over the fatty oil, it the latter is used, preferably inlarge excess.

I give the following classification of antiseptic components, as theterm-is employed in the present' case, the term including substanceswhich are directly antiseptic, as well as substances which when used inmixtures of the type set forth 5 become antiseptic or which liberate orform or In making this generate or produce or are converted intosubstances which have antiseptic activity. In this classification I alsogive a convenient mode of putting the said antiseptic material intosolution, dispersion or quasi-solution, and I also give a convenientsafe, effective and practical percentage of the antiseptic substances,based on the amount of the vehicle (these being illustrative, withoutlimiting the invention thereto, except as specified in the appendedclaims) (1) Elemental sulphur (in triethanolamine at 120 F.). 10%.

(2) Elemental iodine (in triethanolamine at 120 F.). 0.02%.

(3) Phenolic bodies, suitable effective examples being phenol (carbolic.acid) and cresol (or cresylic acid). These'can be dissolved intriethanolamine at 90 to 120? F. 0.1% to 0.2%.

(4.) Resorcin and its derivatives, e. 3. highamples being bismuth betanaphtholate and blsmuth tribromphenate and potassium sodiumbismutho-tartrate which can be dissolved in oleic acid at 105 F. to 110F. 2%.

(5d) Metallo-organic aluminum compounds,-

examples being aluminum phenol-sulphonate and aluminumbetaenaphthol-disulphonate, which can be dissolved in oleic acid at 105F. 1%.

(5e) Metallo-organic compounds of antimony,' an example being antimonythio-glycol-amide,

which can be dissolved in the mineral oil at room temperature, say 75 F.0.2% is suitable.

(6) Such chlorine compounds as para-sulphondichlor-amido-benzolc acid orpara-toluene-sulphon-dlchlor-amide, which can be dissolved intriethanolamine at 80 F. 2%.

(7) As compounds of oxy-quinolin, suitable for use, I mention thesulphate or benzoates of oxyquinolin, which can be dissolved in theoleic acid at 84 F. 2%.

(8) Typical of the sulphur compounds effective for the purpose isammontium sulpho-ichthyolate which can be dissolved in triethanolamineat 120 F. Or it can be dissolved in the mineral oil. Up to about 10% canbe used.

(9) Trichloro-organic compounds containing an OH group, examples beingtrichioro-butyl alcohol and trichloro-phenol. These can be dissolved intriethanolamine at 80 F. 2%.

(10) Antiseptically active dyes containing the methyl group, examplesbeing 3:6 diamino-IO- methyl-acridinum chloride mono-hydrochloride andpentaand hexa-methyl-para-rosaniline. These can be dissolved in oleicacid at 80 C. 0.1%.

(11) Organic iodine compounds other than iodo-benzoic acid, an examplebeing di-iodohydroxy-propane or diiodhydrine, or also iothion, which canbe dissolved in triethanolamine at 120 F. .2%.

(12) Fatty acid esters of phenolic bodies, such as cresyl acetate can beused, dissolved in the mineral oil at room temperature. 0.1%.

All of the above mentioned compositions, can be used for the treatmentof vaginal disorders, one or the other being more suitable, dependingupon the organisms present, causing the trouble. Thus for instance thearsenic compounds are highly suitable for the treatment of tricomonasvaginalis, the elemental iodine and the organic iodine compounds wouldbe suitable to use in cases of cervical erosion and vaginalis, theresorcin derivatives being suitable as hygienic cleansers, and forapplication against minor infections.

The preferred way of compounding the medicines is similar in all cases,namely first dissolve the antiseptic in the particular one of thecomponents referred to above, after which the oleic acid is well mixedwith the mineral oil, and the triethanolamine subsequently added andwell mixed. In producing the medicine, the following hasbeen found to bethe most advantageous procedure. The oleic acid may first be warmed up,say to about 120 F., and the mineral oil is then added, and the mixturewell stirred for 10 or 15 minutes. After this the triethanolamine isadded and well stirred, for 10 minutes or up to onehalf hour. Theaddition of the triethanolamine first gives a somewhat milky mixture,and upon continuing the stirring, the mass becomes thoroughly clear; Thestirring is preferably continued until the solution has become clear,and the reactions will have been sufllciently completed when thesolution has become clear. The fatty oil, if this is to be employed, canbe previously mixed with the mineral oil, or can be added to the mixtureafter addition of the mineral oil. -It will be understood that in theabove formula, for the preparation of the medicine, it is immaterial(from the standpoint of procedure) which one of the components of thevehicle contains the antiseptic, and it will be further understood thatwater is not added to the material or to the finished medicine, and itis important that the components be free from moisture. In making up themedicine, it is advisable particularly in wet weather or when theatmosphere is highly charged with moisture, to put the completedmedicine into a sealed receptacle, for example into the collapsiblemetal tube in which it is to be shipped and sold promptly afterpreparation. It is important also that the components be used in asubstantially or completely anhydrous condition, in or-= .acids such asstearic.

I present,

der to get a mixed oil having a considerable ailinity for moisture, andfreely liquid.

The completed medicine is in all cases a viscous oily liquid, the colordepending upon the particular antiseptic employed.

In the above formula, oleic acid was referred to. It will be understoodthat for producing a mixture of higher viscosity, a small amount of theoleic acid can be substitutedby solid fatty I would not ordinarilyrecommend substituting more than one-fifth of the oleic acid by stearic.

The medicinal mineral oil can be the widely used variety sold as a mildlaxative, being a water-white liquid, having a specific gravity of about0.84, and a Saybolt viscosity at 100 C. about 150, and free fromunsaturated constituents. Other similar oils can be used.

The fatty oil, e. g. cottonseed oil or olive oil if used, may be theusual well refined dehydrated edible grades. In place of these oils,other well refined liquid fatty oils can be used, for example soybeanoil, peanut oil, sesame oil, perilla oil or the like, all preferably inthe well refined dehydrated condition and substantially free from odors.If the fatty oil used contains considerable free fatty acid, slightlymore of the said oil and slightly less of the oleic acid can be suitablyemployed. The use of the well refined oil and of the well refined freefatty acid are however more desirable, as giving a product more freeforms a mass of jelly-like consistency which strongly adheres to wetmucous surfaces,

The action of the oily medicine when it is brought into contact withwater (or aqueous liq uids) containing bacteria or other livingvmicroorganisms, has been carefully studied, under the microscope. Theoily material bursts into the aqueous liquid forming billows of softjelly-like consistency drawing into-itself these micro-organisms, tocompletely envelop the same. Following this action, the jelly stiffenssomewhat imprisoning the said micro-organisms, which are therebydestroyed. This action takes place irrespective of what forms ofmicro-organisms are whether coll-bacillus, staphylococci, spirochaetae,streptococci, spores, spermatazoa or various mixed cultures, or in factany living organisms. The oily mixture made in substantially the aboveproportions, has an affinity for water, or in other words, ishydrophilic" and the Jelly formed is a hydrophilic colloid.

The medicine is particularly advantageous for application to mucoussurfaces of the vagina from which liquids are being exuded, whether innormal healthy condition or in a diseased condition.

In the above description of the complete medicine I have described theuse of one or more of a considerable number of antiseptic substances,which are suitable for use, as antiseptics. In some instances, thevehicle alone without the addition of the antiseptic substances, or anyof them, can be employed. Thus for instance, the vehicle alone, i. e.without the addition of any antiseptic substances thereto, can be usedas a vaginal cleanser, or for clearing up minor conditions where thereis no deep-seated infection. For this purpose, a small quantity of theoily material, for example 3 to 10 cc. of the same can be introducedinto the vagina, and allowed to read:

with the secretion therein, and form the'jellylike mass as referred toabove. of the said jelly of course picks up any bacteria or otherorganisms present or introduced, as well' as solid materials, debris orother foreign matter, all of which would be removed on flushing out witha warm water douche, the jelly of course carrying away with it anysolids or bacteria contained therein.

The vehicle itself, either with or without the addition of antisepticsubstances, is also suitable for application to burns or to other skinaffections in which there is a more or less great amount of discharge ofwatery excretions. The use of the material for this purpose isparticularly suitable in cases where it is not desired to use bandagesor the like, because the jelly-like mass formed will readily adhere tothe skin, as well as to mucous surfaces, without the aid of anybandages, tampons, or the like. For this purpose, it will be obviousthat no large amounts of water, or aqueous liquids are to be applied.This gives a protection over tender surfaces where there is an aqueoussecretion.

No claim is made herein specifically on the use of iodobenzoic acid asthe antiseptic in a vehicle containing fatty ofl, as described above,that subject matter being claimed in a copending case. Serial No.124,135.

I claim:-

1. The herein described topical antiseptic medicine suitable for thetreatment of vaginal disorders, which is iree from water and adapted,upon coming into contact with aqueous secretions on mucous surfaces, todraw said secretions into itself, thereby forming a jelly-like masswhich will readily adhere to said mucous surfaces, said medicine beingin the form of a mobile oily liquid, having the appearance andconsistency of a substantially clear liquid oil, and the vehicle ofwhich medicine is composed essentially of an oil and the reactionproduct of triethanolamine and a higher fatty acid, the oil in saidvehicle being composed in major part at least of a well purifled liquidpetroleum oil, and the amount of said oil being over 0.75 and less than1.2 times the combined amount of triethanolamine and said higher fattyacid, said vehicle carrying dissolved therein an antiseptic componentother than iodobenzoic acid, such topical medicine, when applied to amucous surface of the vagina form-.

ing thereon an adherent Jelly-like clinging mass. 2. The hereindescribed topical antiseptic medicine suitable for treating vaginaldisorders, which is free from water and adapted, upon coming intocontact with aqueous secretions on mucous surfaces, to draw saidsecretions into itself, thereby forming a Jelly-libs mass which willreadily adhere to Q medicinebeingintheformofamobilooilyliquid,

The formation having the appearance and consistency of a substantiallyclear liquid OH, and the vehicle of which medicine is composedessentially of an oil and the reaction product of triethanolamine and ahigher fatty acid, the oil in said vehicle being composed in-major partat least of a well purified liquid petroleum oil, and the amount of saidoilbeing over 0.75 and less than 1.2 times the combined amount oftriethanolamine and said higher fatty acid, said vehiclev carryingdissolved therein a metallo-organic compound of mercury as anantiseptic, such topical medicine, when applied to a mucous'surface ofthe vagina forming thereon an adherent jelly-like clinging mass.

3. The herein described topical antiseptic medicine suitable for thetreatment of vaginal disorders, which'is free from water and adapted,upon coming into contact with aqueous secretions on mucous surfaces, todraw said secretions into itself, thereby forming a jelly-like masswhich will readily adhere to said mucous surfaces, said medicine beingin the form of a mobile oily liquid,

' having the appearance and consistency of a substantially clear liquidoil, and the vehicle of which medicine is composed essentially of an oiland the reaction product of triethanolamine and a higher fatty acid, theoil in said vehicle being composed in, major part at least of a wellpurified liquid petroleum oil, and the amount of said oil being over0.75 and less than 1.2 times the combined amount oftriethanolamine andsaid higher fatty acid, said vehicle carrying dissolved therein aphenolic body as an antiseptic, such topical medicine, when applied to amucous surface of the vagina forming thereon an adherent jelly-likeclinging mass. v

4. A topical antiseptic medicine as covered in claim 1, in which the oilpresent is a mixture of a well purified petroleum oil and a fatty oil,theformer being in excess over the latter.

5. The herein described topical agent adapted for the treatment ofvaginal disorders, which is free from water and adapted, upon cominginto contact with aqueous secretions on mucous surfaces of the vaginalcavity, to draw said secretions into itself together with any extraneoussolids and organisms therein, thereby forming a jelly-like mass whichwill readily adhere to said mucous surfaces, said agent being inthe-form of a mobfle oily liquid, having the appearance and consistencyof a substantially clear liquid oil, and composed at least largely of anoil and the reaction product of trietbanolamine and a higher fatty acid,the oil in said agent being composed in major part at least of a wellpurified liquid petroleum oil, and the amount of said oil being over0.75 and below 1.2 times the combined amount of triethsnolamine and'saidhigher fatty FRANK J. BICKENI-IEUSER.

said mucous surfaces, sci

